Use of estrogens and delta-gonadien-21-Ol-3,20-diones for treating insulin dependent and non-insulin dependent diabetes

Abstract

Analysis of full-blood glucose, serum insulin, serum triglycerides and total serum cholesterol were performed. Glucose levels in blood samples from the oral glucose tolerance test were used for calculation of the incremental Area Under the Curve (AUC0-120 min-baseline). All data are expressed as percentage change of vehicle treated animals (cf. FIGS. 1 and 2).

Description

FIELD OF THIS INVENTIONThe present invention relates to the use of a combination of estrogens or SERMs with delta-gonadien-21-ol-3,20-diones for treating diabetes, particularly type II diabetes. The present invention also embraces pharmaceutical compositions and kits comprising these compounds and methods of using the compounds and their pharmaceutical compositions.BACKGROUND OF THIS INVENTIONDiabetes mellitus is a systemic disease characterized by disorders in the actions of insulin and other regulatory hormones in the metabolism of carbohydrates, fats and proteins, and in the structure and function of blood vessels. The primary symptom of diabetes is hyperglycemia, often accompanied by glucosuria, the presence in urine of large amounts of glucose, and polyuria, the excretion of large volumes of urine. Additional symptoms arise in chronic or long standing diabetes. These symptoms include degeneration of the walls of blood vessels. Although many different organs are affected by thes...

Examples

examples

Conjugated estrogens may be obtained following the process described in U.S. Pat. No. 2,720,483 or U.S. Pat. No. 2,565,115, which are incorporated herein by reference.

The compound having the formula II ##STR11##

may be prepared as described in U.S. Pat. No. 4,273,771. The compound of formula II is called trimegestone.

An example of a tablet contains a conjugated estrogen (0,6 mg) and a compound of formula II (2,4 mg) formulated with pharmaceutically acceptable carriers to provide a medicament for oral administration according to conventional methods. The formulation further include the following diluents, fillers, emulsifiers, preservatives, buffers and / or excipients, that is calcium phosphate tribasic, calcium sulfate, canauba wax, cellulose, glyceryl monooleate, lactose, magnesium stearate, methylcellulose, pharmaceutical glaze, polyethylen glycol, sucrose, povidone, titanium dioxide and red ferric oxide. One skilled in this art may formulate the tablet composition in an appropriate...

FIELD OF THIS INVENTIONThe present invention relates to the use of a combination of estrogens or SERMs with delta-gonadien-21-ol-3,20-diones for treating diabetes, particularly type II diabetes. The present invention also embraces pharmaceutical compositions and kits comprising these compounds and methods of using the compounds and their pharmaceutical compositions.BACKGROUND OF THIS INVENTIONDiabetes mellitus is a systemic disease characterized by disorders in the actions of insulin and other regulatory hormones in the metabolism of carbohydrates, fats and proteins, and in the structure and function of blood vessels. The primary symptom of diabetes is hyperglycemia, often accompanied by glucosuria, the presence in urine of large amounts of glucose, and polyuria, the excretion of large volumes of urine. Additional symptoms arise in chronic or long standing diabetes. These symptoms include degeneration of the walls of blood vessels. Although many different organs are affected by thes...

Examples

examples

Conjugated estrogens may be obtained following the process described in U.S. Pat. No. 2,720,483 or U.S. Pat. No. 2,565,115, which are incorporated herein by reference.

The compound having the formula II ##STR11##

may be prepared as described in U.S. Pat. No. 4,273,771. The compound of formula II is called trimegestone.

An example of a tablet contains a conjugated estrogen (0,6 mg) and a compound of formula II (2,4 mg) formulated with pharmaceutically acceptable carriers to provide a medicament for oral administration according to conventional methods. The formulation further include the following diluents, fillers, emulsifiers, preservatives, buffers and / or excipients, that is calcium phosphate tribasic, calcium sulfate, canauba wax, cellulose, glyceryl monooleate, lactose, magnesium stearate, methylcellulose, pharmaceutical glaze, polyethylen glycol, sucrose, povidone, titanium dioxide and red ferric oxide. One skilled in this art may formulate the tablet composition in an appropriate...

Images